Description
Cas：579515-63-2
Product Information：
GW806742X is a Mixed Lineage Kinase Domain-Like protein (MLKL) inhibitor which binds the MLKL pseudokinase domain with a Kd value of 9.3 μM and has anti-necroptosis activity. GW806742X has activity against VEGFR2.
IC50 & Target: Kd: 9.3 μM (MLKL)[1]
Molecular Weight: 573.55
Formula: C₂₅H₂₂F₃N₇O₄S
Smiles Code:
O=S(C1=CC=CC(NC2=NC=CC(N(C)C3=CC=C(NC(NC4=CC=C(OC(F)(F)F)C=C4)=O)C=C3)=N2)=C1)(N)=O
Shipping:
Room temperature in continental US; may vary elsewhere.
Storage:
4°C, sealed storage, away from moisture
In Vitro:
GW806742X (0.1-10000 nM) rescues 50% of wild-type mouse dermal fibroblasts (MDFs) from TSQ-induced necroptosis with an IC50< 50 nM when 1 ng/mL TNF is used.
GW806742X (1 μM) retards MLKL translocation to the membrane.
References：
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Hildebrand JM, et al. Activation of the pseudokinase MLKL unleashes the four-helix bundle domain to induce membrane localization and necroptotic cell death. Proc Natl Acad Sci U S A. 2014 Oct 21;111(42):15072-7.
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Yan B, et al. Discovery of a new class of highly potent necroptosis inhibitors targeting the mixed lineagekinase domain-like protein. Chem Commun (Camb). 2017 Mar 28;53(26):3637-3640.
Products are for research use only. Not for human use.
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